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PF-5081090

CAS No. : 1312473-63-4

MCE 站：PF-5081090

产品活性：PF-5081090 (LpxC-4) 是一种强效的 LpxC 抑制剂，具有广谱、快速的杀菌活性。PF-5081090 能够调节革兰氏阴性菌中脂类 A 生物合成。

研究领域：Anti-infection

作用靶点：Antibiotic  |  Bacterial

In Vitro: PF-5081090 shows strong potency against a broad spectrum of Gram-negative pathogens with IC₅₀s of 1.1 nM (P. aeruginosa), 0.069 nM (K. pneumonia) ａnd MIC₉₀s of 1 μg/mL (P. aeruginosa, K. pneumoniae), 0.25 μg/mL (E. coli), 0.5 μg/mL (Enterobacter spp), 2 μg/mL (S. maltophilia).
PF-5081090 (0.25 μg/mL; 0-50 h) demonstrates sustained bactericidal activities against P. aeruginosa UC12120 (A), PA-1955 (B), ａnd K. pneumoniae KP-1487.
PF-5081090 (32 mg/L) increases antibiotic susceptibility in Acinetobacter baumannii with rifampicin, vancomycin, azithromycin, imipenem ａnd amikacin.
PF-5081090 (32 mg/L) inhibits lipid A biosynthesis, ａnd significantly increases cell permeability in A. baumannii.

In Vivo: PF-5081090 (8.75, 75, 300 mg/kg; s.c.; single dose) exhibits a exposure increasing in linear manner across the dose range in mice, with area under the concentration-time curve (AUC) ａnd maximum concentration of drug in serum (C_max) increasing with a proportional increase in dose.
PF-5081090 shows potent efficacies against sentinel strains of P. aeruginosa ａnd K. pneumonia in CD-1 mice, with effective dose (ED₅₀) ranging from 7.4-55.9 mg/kg (against acute septicemia model), <25 mg/kg (against pneumonia model), ａnd 16.8 mg/kg (against neutropenic thigh model) in mice infected with P. aeruginosa PA-1950.
Pharmacokinetics of PF-5081090 in CD-1 mice^a

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